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[PMID]:24385009
[Au] Autor:Khomenko T; Deng X; Ahluwalia A; Tarnawski A; Patel KN; Sandor Z; Szabo S
[Ad] Endereço:VA Medical Center, (05/113) 5901 East 7th Street, Long Beach, CA, 90822-5201, USA.
[Ti] Título:STAT3 and importins are novel mediators of early molecular and cellular responses in experimental duodenal ulceration.
[So] Source:Dig Dis Sci;59(2):297-306, 2014 Feb.
[Is] ISSN:1573-2568
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that directly upregulates VEGF, Ref-1, p21, and anti-apoptotic genes such as Bcl-xL. In this study, we hypothesized that STAT3 signaling is activated and provides a critical protective role that is required for enterocyte survival during the early phases of cysteamine-induced duodenal ulcers. METHODS: We studied the effect of inhibition of STAT3 activity on cysteamine-induced duodenal ulcers in rats and egr-1 knockout mice using STAT3/DNA binding assay, immunohistochemistry, immunoblot, and quantitative reverse transcriptase PCR analyses. RESULTS: We found that G-quartet oligodeoxynucleotides T40214, a specific inhibitor of STAT3/DNA binding, aggravated cysteamine-induced duodenal ulcers in rats 2.8-fold (p < 0.05). In the pre-ulcerogenic stage, cysteamine induced STAT3 tyrosine phosphorylation, its translocation to nuclei, an increased expression and nuclear translocation of importin α and ß in the rat duodenal mucosa. Cysteamine enhanced the binding of STAT3 to its DNA consensus sequences at 6, 12, and 24 h after cysteamine by 1.5-, 1.8-, and 3.5-fold, respectively, and activated the expression of STAT3 target genes such as VEGF, Bcl-xL, Ref-1, and STAT3-induced feedback inhibitor, a suppressor of cytokine signaling 3. We also demonstrated that egr-1 knockout mice, which are more susceptible to cysteamine-induced duodenal ulcers, had lower levels of STAT3 expression, its phosphorylation, expression of importin α or ß, and STAT3/DNA binding than wild-type mice in response to cysteamine. CONCLUSIONS: Thus, STAT3 represents an important new molecular mechanism in experimental duodenal ulceration.
[Mh] Termos MeSH primário: Úlcera Duodenal/metabolismo
Duodeno/metabolismo
Fator de Transcrição STAT3/metabolismo
Transdução de Sinais
alfa Carioferinas/metabolismo
beta Carioferinas/metabolismo
[Mh] Termos MeSH secundário: Transporte Ativo do Núcleo Celular
Animais
Apoptose
Cisteamina
Modelos Animais de Doenças
Úlcera Duodenal/induzido quimicamente
Úlcera Duodenal/genética
Úlcera Duodenal/patologia
Úlcera Duodenal/prevenção & controle
Duodeno/efeitos dos fármacos
Duodeno/patologia
Proteína 1 de Resposta de Crescimento Precoce/deficiência
Proteína 1 de Resposta de Crescimento Precoce/genética
Epirizol
Feminino
Regulação da Expressão Gênica
Camundongos
Camundongos Knockout
Oligodesoxirribonucleotídeos/farmacologia
Fosforilação
Ratos
Ratos Sprague-Dawley
Fator de Transcrição STAT3/antagonistas & inibidores
Transdução de Sinais/efeitos dos fármacos
Fatores de Tempo
Tirosina
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Early Growth Response Protein 1); 0 (Egr1 protein, mouse); 0 (GQ-ODN T40214); 0 (Oligodeoxyribonucleotides); 0 (STAT3 Transcription Factor); 0 (Stat3 protein, mouse); 0 (Stat3 protein, rat); 0 (alpha Karyopherins); 0 (beta Karyopherins); 3B46O2FH8I (Epirizole); 42HK56048U (Tyrosine); 5UX2SD1KE2 (Cysteamine)
[Em] Mês de entrada:1404
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:140104
[St] Status:MEDLINE
[do] DOI:10.1007/s10620-013-2807-6


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[PMID]:22084084
[Au] Autor:Rovira M; Huang W; Yusuff S; Shim JS; Ferrante AA; Liu JO; Parsons MJ
[Ad] Endereço:Department of Surgery, and McKusick-Nathans Institute for Genetic Medicine, The Johns Hopkins University, Baltimore, MD 21205, USA.
[Ti] Título:Chemical screen identifies FDA-approved drugs and target pathways that induce precocious pancreatic endocrine differentiation.
[So] Source:Proc Natl Acad Sci U S A;108(48):19264-9, 2011 Nov 29.
[Is] ISSN:1091-6490
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Pancreatic ß-cells are an essential source of insulin and their destruction because of autoimmunity causes type I diabetes. We conducted a chemical screen to identify compounds that would induce the differentiation of insulin-producing ß-cells in vivo. To do this screen, we brought together the use of transgenic zebrafish as a model of ß-cell differentiation, a unique multiwell plate that allows easy visualization of lateral views of swimming larval fish and a library of clinical drugs. We identified six hits that can induce precocious differentiation of secondary islets in larval zebrafish. Three of these six hits were known drugs with a considerable background of published data on mechanism of action. Using pharmacological approaches, we have identified and characterized two unique pathways in ß-cell differentiation in the zebrafish, including down-regulation of GTP production and retinoic acid biosynthesis.
[Mh] Termos MeSH primário: Diferenciação Celular/efeitos dos fármacos
Descoberta de Drogas/métodos
Células Secretoras de Insulina/citologia
Células Secretoras de Insulina/efeitos dos fármacos
Preparações Farmacêuticas/metabolismo
[Mh] Termos MeSH secundário: Acetanilidas/farmacologia
Animais
Animais Geneticamente Modificados
Ácidos Cafeicos/farmacologia
Linhagem Celular Tumoral
Proliferação Celular
Primers do DNA/genética
Dimetil Sulfóxido
Relação Dose-Resposta a Droga
Epirizol/farmacologia
Imunofluorescência
Proteínas de Fluorescência Verde
Guanosina Trifosfato/biossíntese
Proteína HMGB1/metabolismo
Larva/efeitos dos fármacos
Microscopia Confocal
Ácido Micofenólico/farmacologia
Reação em Cadeia da Polimerase em Tempo Real
Ácidos Sulfanílicos/farmacologia
Tretinoína/metabolismo
Peixe-Zebra
p-Aminoazobenzeno/análogos & derivados
p-Aminoazobenzeno/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Acetanilides); 0 (Caffeic Acids); 0 (DNA Primers); 0 (HMGB1 Protein); 0 (N-(4-(3-(3,4-dihydroxyphenyl)acryloyl)phenyl)-2-(thiophen-2-yl)acetamide); 0 (Pharmaceutical Preparations); 0 (Sulfanilic Acids); 147336-22-9 (Green Fluorescent Proteins); 2481-94-9 (C.I. Solvent Yellow 56); 3B46O2FH8I (Epirizole); 5688UTC01R (Tretinoin); 57X2AH42T1 (p-Aminoazobenzene); 86-01-1 (Guanosine Triphosphate); HU9DX48N0T (Mycophenolic Acid); YOW8V9698H (Dimethyl Sulfoxide)
[Em] Mês de entrada:1201
[Cu] Atualização por classe:161208
[Lr] Data última revisão:
161208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:111116
[St] Status:MEDLINE
[do] DOI:10.1073/pnas.1113081108


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[PMID]:15146935
[Au] Autor:Tanaka J; Iida H; Abe M; Yuda Y; Inoue S; Okabe S
[Ad] Endereço:Pharmacology Department, Drug Research Laboratories, Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan. junko_tanaka@meiji.co.jp
[Ti] Título:Gastric antisecretory and anti-ulcer effect of ME3407, a new benzimidazole derivative, in rats.
[So] Source:Arzneimittelforschung;54(4):221-9, 2004.
[Is] ISSN:0004-4172
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The effects of a new benzimidazole derivative, ME3407 (n-butyl-2-(thiazolo-[5,4-b]pyrid-2-yl) sulfinylacetate, CAS 133903-90-9), on gastric acid secretion and gastric and duodenal ulcers in rats were examined. ME3407, given orally, inhibited dose-dependently (0.3-30 mg/kg) the incidence of gastric lesions such as Shay ulcers, and water-immersion stress-, acetylsalicylic acid (ASA)- and histamine-induced erosions. In addition, ME3407 showed marked therapeutic effect on HCl- and ASA-induced lesions. In the lumen-perfused rats, oral administration of ME3407 inhibited dose-dependently (1-100 mg/kg) gastric acid secretion induced by histamine and tetragastrin with ED50 values of 3.02 and 3.37 mg/kg, respectively. Oral administration of ME3407 at a dose of 30 mg/kg also inhibited the elevation of serum gastrin level. The development of duodenal ulcers caused by mepirizole and systeamine was also potently inhibited by ME3407 at an oral dose of 0.1-30 mg/kg. However, when given at 30 mg/kg intraduodenally, subcutaneously or intravenously, ME3407 did not inhibit these acutely induced gastric elosion and acid output. ME3407 was not detected in the serum upon oral administration. These results indicated that ME3407 was active only by oral administration, and exerts direct action on the ulcers and acid secretion from the gastric membrane.
[Mh] Termos MeSH primário: Antiulcerosos/farmacologia
Benzimidazóis/farmacologia
Ácido Gástrico/secreção
Mucosa Gástrica/secreção
Piridinas/farmacologia
Tiazóis/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios
Aspirina
Cisteamina
Úlcera Duodenal/induzido quimicamente
Úlcera Duodenal/prevenção & controle
Epirizol
Fístula Gástrica/fisiopatologia
Mucosa Gástrica/efeitos dos fármacos
Gastrinas/sangue
Histamina
Imersão/efeitos adversos
Indometacina
Masculino
Pepsina A/secreção
Piloro/fisiologia
Ratos
Úlcera Gástrica/induzido quimicamente
Úlcera Gástrica/prevenção & controle
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Anti-Ulcer Agents); 0 (Benzimidazoles); 0 (Gastrins); 0 (ME 3407); 0 (Pyridines); 0 (Thiazoles); 3B46O2FH8I (Epirizole); 5UX2SD1KE2 (Cysteamine); 820484N8I3 (Histamine); EC 3.4.23.1 (Pepsin A); R16CO5Y76E (Aspirin); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:0406
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040519
[St] Status:MEDLINE


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[PMID]:14658885
[Au] Autor:Escrivà E; García-Lozano J; Martínez-Lillo J; Nuñez H; Server-Carrió J; Soto L; Carrasco R; Cano J
[Ad] Endereço:Departament de Química Inorgànica, Universitat de València, c/Vicent Andrés Estellés, s/n, 46100 Burjassot (València), Spain. escriva@uv.es
[Ti] Título:Synthesis, crystal structure, magnetic properties, and theoretical studies of [(Cu(mepirizole)Br)2(mu-OH)(mu-pz)] (mepirizole=4-methoxy-2-(5-methoxy-3-methyl-1H-pyrazol-1-yl)-6-methylpyrimidine; pz=pyrazolate), a novel mu-pyrazolato-mu-hydroxo-dibridged copper(II) complex.
[So] Source:Inorg Chem;42(25):8328-36, 2003 Dec 15.
[Is] ISSN:0020-1669
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A novel mu-pyrazolato-mu-hydroxo-dibridged copper(II) complex has been synthesized and structurally characterized: [(Cu(mepirizole)Br)2(mu-OH)(mu-pz)] (mepirizole=4-methoxy-2-(5-methoxy-3-methyl-1H-pyrazol-1-yl)-6-methylpyrimidine; pz=pyrazolate). The title compound crystallizes in the monoclinic system, space group P2(1)/c, with a=15.618(2) A, b=15.369(3) A, c=16.071(3) A, and beta=112.250(1) degrees. The structure is built up of dinuclear [(Cu(mepirizole)Br)2(mu-OH)(mu-pz)] units with five-coordinated copper(II) ions (CuBrN3O chromophores) linked by mu2-OH and mu2-pyrazolato bridges that are well separated from each others. The intramolecular copper-copper distance is 3.378(3) A. Magnetic susceptibility data show that the copper atoms are strongly antiferromagnetically coupled with J=-770 cm(-1). The obtained triplet-singlet energy gap is compared with those reported for a series of related dimers. The strong antiferromagnetic coupling arising from the complementarity of the hydroxo and pyrazolato bridges has been discussed on the basis of DFT calculations.
[Mh] Termos MeSH primário: Epirizol/química
Ferro/química
[Mh] Termos MeSH secundário: Fenômenos Químicos
Química Física
Cristalografia por Raios X
Indicadores e Reagentes
Ligantes
Magnetismo
Modelos Moleculares
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Indicators and Reagents); 0 (Ligands); 3B46O2FH8I (Epirizole); E1UOL152H7 (Iron)
[Em] Mês de entrada:0404
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:031209
[St] Status:MEDLINE


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[PMID]:12270242
[Au] Autor:Onoa GB; Moreno V
[Ad] Endereço:Departament de Química Inorgànica, Universitat de Barcelona, Avgda Diagonal 647, 08028 Barcelona, Spain. virtudes.moreno@qi.ub.es
[Ti] Título:Study of the modifications caused by cisplatin, transplatin, and Pd(II) and Pt(II) mepirizole derivatives on pBR322 DNA by atomic force microscopy.
[So] Source:Int J Pharm;245(1-2):55-65, 2002 Oct 01.
[Is] ISSN:0378-5173
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Modifications of the structure of pBR322 DNA caused by interaction with cisplatin, transplatin and Pd(II) and Pt(II) mepirizole derivatives were studied. The compounds were incubated with the plasmid DNA for 24 h at 37 degrees C and then observed with an atomic force microscope. Circular DNA was used because the small tertiary structural changes are easy to monitor. Likewise, its superhelical nature mimics DNA better than certain forms of intracellular DNA such as chromatin. AFM images clearly reveal that the complexes induce changes in the topological forms of fully relaxed pBR322 DNA. Most of the compounds produce a more compact DNA structure with modified writhing number. Analysis of gel migration of the relaxed pBR322 DNA incubated with the platinum complexes provides complementary information, which is in good agreement with AFM results.
[Mh] Termos MeSH primário: Epirizol/análogos & derivados
Epirizol/química
Paládio
Plasmídeos/química
Compostos de Platina/química
[Mh] Termos MeSH secundário: Antineoplásicos/química
Cisplatino/química
Eletroforese em Gel Bidimensional
Seres Humanos
Técnicas In Vitro
Microscopia de Força Atômica
Conformação de Ácido Nucleico
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Platinum Compounds); 14913-33-8 (transplatin); 3B46O2FH8I (Epirizole); 5TWQ1V240M (Palladium); Q20Q21Q62J (Cisplatin)
[Em] Mês de entrada:0212
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020925
[St] Status:MEDLINE


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[PMID]:10707886
[Au] Autor:Takeuchi K; Sugamoto S; Suzuki K; Kawauchi S; Furukawa O
[Ad] Endereço:Department of pharmacology and Experimental Therapeutics, Kyoto Pharmaceutical University, Yamashina, Japan. takeuchi@mb.kyoto-phu.ac.jp
[Ti] Título:Effects of endothelin-1 on duodenal bicarbonate secretion and mucosal integrity in rats.
[So] Source:Chin J Physiol;42(3):129-35, 1999 Sep 30.
[Is] ISSN:0304-4920
[Cp] País de publicação:China (Republic : 1949- )
[La] Idioma:eng
[Ab] Resumo:Effects of endothelin-1 on gastric acid secretion, duodenal HCO3- secretion, and duodenal mucosal integrity were investigated in anesthetized rats, in comparison with those of TY-10957, a stable analogue of prostacyclin. A rat stomach mounted on an ex-vivo chamber or a proximal duodenal loop was perfused with saline, and gastric acid or duodenal HCO3- secretion was measured using a pH-stat method and by adding 100 mM NaOH or 10 mM HCl, respectively. Duodenal lesions were induced by mepirizole (200 mg/kg) given subcutaneously. Intravenous administration of endothelin-1 (0.6 and 1 nmol/kg) caused an increase of duodenal HCO3- secretion with concomitant elevation of blood pressure; this effect was antagonized by co-administrahon of BQ-123 (ET(A) antagonist; 3 mg/kg, i.v.) and significantly mitigated by vagotomy. Likewise, endothelin-1 caused a significant decrease in histamine-stimulated acid secretion, and this effect was also significantly antagonized by BQ-123. Although TY-10957 (10 and 30 mg/kg, i.v.) produced a temporal decrease of blood pressure, this agent caused not only an increase of duodenal HCO3- secretion, independent of vagal nerves, but also a decrease of acid secretion as well. In addition, both endothelin-1 and TY-10957 significantly prevented mepirizole-induced duodenal lesions at the doses that caused an increase of duodenal HCO3- secretion and a decrease of gastric acid secretion. These results suggest that endothelin-1 affects the duodenal mucosal integrity by modifying both gastric acid and duodenal HCO3- secretions, the effects being mediated by ET(A) receptors.
[Mh] Termos MeSH primário: Bicarbonatos/metabolismo
Duodeno/efeitos dos fármacos
Duodeno/secreção
Endotelina-1/farmacologia
Mucosa Intestinal/secreção
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides
Antiulcerosos/farmacologia
Anti-Hipertensivos/farmacologia
Úlcera Duodenal/induzido quimicamente
Úlcera Duodenal/metabolismo
Úlcera Duodenal/patologia
Duodeno/patologia
Epirizol
Epoprostenol/análogos & derivados
Epoprostenol/metabolismo
Epoprostenol/farmacologia
Ácido Gástrico/metabolismo
Concentração de Íons de Hidrogênio
Masculino
Peptídeos Cíclicos/farmacologia
Ratos
Ratos Sprague-Dawley
Vagotomia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Anti-Ulcer Agents); 0 (Antihypertensive Agents); 0 (Bicarbonates); 0 (Endothelin-1); 0 (Peptides, Cyclic); 117028-28-1 (TY 10957); 3B46O2FH8I (Epirizole); DCR9Z582X0 (Epoprostenol); S2A8YZM151 (cyclo(Trp-Asp-Pro-Val-Leu))
[Em] Mês de entrada:0003
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:000309
[St] Status:MEDLINE


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[PMID]:10535682
[Au] Autor:Sohn SK; Chang MS; Choi WS; Kim KB; Woo TW; Lee SB; Chung YK
[Ad] Endereço:Pharmacology and Toxicology Laboratory, Yung-Jin Pharmaceutical Co. Ltd., Hwasung-Kun, Kyunggi-Do, South Korea.
[Ti] Título:Biochemical and pharmacological characteristics of a newly synthesized H+-K+ ATPase inhibitor, YJA20379-1, 2-amino-4,5-dihydro-8-phenylimidazole[2,1-b]thiazolo[5,4-g]benzothiazol e.
[So] Source:Can J Physiol Pharmacol;77(5):330-8, 1999 May.
[Is] ISSN:0008-4212
[Cp] País de publicação:Canada
[La] Idioma:eng
[Ab] Resumo:The biochemical and pharmacological characteristics of a newly synthesized H+-K+ ATPase inhibitor, 2-amino-4,5-dihydro-8-phenylimidazole[2,1-b]thiazolo[5,4-g]benzothiazole (YJA20379-1), were investigated. In the pig gastric microsomes, YJA20379-1 inhibited the gastric H+-K+ ATPase regardless of pH condition, IC50 values being 21 and 24 microM at pH 6.4 and 7.4, respectively. The inhibitory activity of YJA20379-1 was antagonized by dithiothreitol treatment but could not be reversed by dilution and washing of the enzyme preparation. In Sprague-Dawley rats, YJA20379-1, administered i.d., p.o, i.v., or s.c., significantly inhibited basal gastric acid secretion, with ED50 values of 4.7, 20.2, 6.3, and 13.4 mg/kg, respectively. The antisecretory action of YJA20379-1 was short lasting (less than 7 h at an oral dosing of 30 mg/kg). Oral administration of YJA20379-1 also prevented the formation of ethanol, indomethacin, and water immersion stress induced gastric lesions and mepirizole-induced duodenal ulcers in rats. Furthermore, YJA20379-1 accelerated the healing of acetic acid induced chronic gastric ulcers in rats. In conclusion, these results suggest that YJA20379-1 has a potent inhibitory activity on the gastric H+-K+ ATPase but much shorter duration of antisecretory action than omeprazole, thereby exerting its anti-ulcer effects partly with cytoprotective activity.
[Mh] Termos MeSH primário: Antiulcerosos/farmacologia
Imidazóis/farmacologia
Inibidores da Bomba de Prótons
Tiazóis/farmacologia
[Mh] Termos MeSH secundário: Animais
Benzotiazóis
Ditiotreitol/farmacologia
Epirizol/toxicidade
Etanol/toxicidade
Feminino
Ácido Gástrico/secreção
Mucosa Gástrica/efeitos dos fármacos
Indometacina/toxicidade
Masculino
Ratos
Ratos Sprague-Dawley
Suínos
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Ulcer Agents); 0 (Benzothiazoles); 0 (Imidazoles); 0 (Proton Pump Inhibitors); 0 (Thiazoles); 0 (YJA 20379-1); 3B46O2FH8I (Epirizole); 3K9958V90M (Ethanol); T8ID5YZU6Y (Dithiothreitol); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:9911
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:991027
[St] Status:MEDLINE


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[PMID]:10474205
[Au] Autor:Onoa GB; Moreno V; Font-Bardia M; Solans X; Pérez JM; Alonso C
[Ad] Endereço:Departament de Química Inorgànica, Universitat de Barcelona, Spain.
[Ti] Título:Structural and cytotoxic study of new Pt(II) and Pd(II) complexes with the bi-heterocyclic ligand mepirizole.
[So] Source:J Inorg Biochem;75(3):205-12, 1999 Jun 30.
[Is] ISSN:0162-0134
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Pd(II) and Pt(II) complexes of formulae [MLCl2], where L = mepirizole, were synthesized and characterized. Two complexes were obtained and studied by different techniques: IR, 1H and 13C NMR and XPS spectroscopies and mass spectrometry (electrospray). The crystal structure of the complex cis-dichloro-4-methoxy-2-(5-methoxy-3-methyl- pyrazol-1-yl)-6-methyl-pyrimidinepalladium(II), [Pd(mep)Cl2], was studied by crystal X-ray diffraction. It consists of discrete molecules with planar geometry. Pd(II) ions are four-coordinated by two mepirizole nitrogen atoms (N1 from the pyrazole ring and N4 from the pyrimidine ring) and two chlorine atoms. The geometry of the PdN2Cl2 chromophore is a distortion of the square-planar coordination. Data from powder pattern X-ray diffraction of cis-dichloro-4-methoxy-2-(5-methoxy-3-methyl-pyrazol-1-yl)-6-methyl- pyrimidineplatinum(II), [Pt(mep)Cl2], demonstrated that the two complexes are isostructural. The cytotoxic activity of both Pd and Pt complexes was checked for six different tumor cell lines and was lower than that of cisplatin. The Pt bound to DNA was also checked and only a low percentage is able to cross the cell membrane.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Epirizol/química
Epirizol/farmacologia
Paládio/química
Platina/química
[Mh] Termos MeSH secundário: Animais
Divisão Celular/efeitos dos fármacos
Linhagem Celular Transformada
Cercopithecus aethiops
Cristalografia por Raios X
Células HL-60
Seres Humanos
Células Jurkat
Ligantes
Camundongos
Análise Espectral
Relação Estrutura-Atividade
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Ligands); 3B46O2FH8I (Epirizole); 49DFR088MY (Platinum); 5TWQ1V240M (Palladium)
[Em] Mês de entrada:9909
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990904
[St] Status:MEDLINE


  9 / 74 MEDLINE  
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Fotocópia
[PMID]:10197495
[Au] Autor:Takeuchi K; Konaka A; Nishijima M; Kato S; Yasuhiro T
[Ad] Endereço:Department of Pharmacology and Experimental Therapeutics, Kyoto Pharmaceutical University, Japan. takeuchi@mb.kyoto-phu.ac.jp
[Ti] Título:Effects of pantoprazole, a novel H+/K+-ATPase inhibitor, on duodenal ulcerogenic and healing responses in rats: a comparative study with omeprazole and lansoprazole.
[So] Source:J Gastroenterol Hepatol;14(3):251-7, 1999 Mar.
[Is] ISSN:0815-9319
[Cp] País de publicação:Australia
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Pantoprazole, 2-[(2-pyridylmethyl) sulphinyl] benzimidazole, is a new substituted benzimidazole that inhibits the parietal cell H+/K+-ATPase. METHODS: In the present study, the anti-secretory and anti-ulcer activities of pantoprazole were compared with those of omeprazole and lansoprazole in rats. RESULTS: Pantoprazole (0.3-3 mg/kg, p.o.) as well as omeprazole (1-10 mg/kg, p.o.) and lansoprazole (1-10 mg/kg, p.o.) dose-dependently decreased both basal acid secretion in pylorus-ligated rats and the stimulated acid secretion induced by mepirizole in acute fistula rats, and the effects of pantoprazole were more potent than those of omeprazole and lansoprazole, the ED50 values for the stimulated acid secretion being 0.8, 2.0 and 1.2 mg/kg, respectively. Neither of these drugs had any effect on duodenal HCO3- secretion. These pump inhibitors prevented the development of duodenal lesions in response to mepirizole in a dose-related manner, the ED50 values for pantoprazole, omeprazole and lansoprazole being 0.4, 2.0 and 1.3 mg/kg, respectively. Likewise, pantoprazole showed the healing promoting action on chronic duodenal ulcers induced by acetic acid, and this effect was also more potent when compared to omeprazole or lansoprazole. CONCLUSIONS: We conclude that pantoprazole exhibited both anti-ulcer and healing promoting effects on duodenal ulcers in rats, and the effects may be attributable to its potent anti-secretory action. Other pump inhibitors such as omeprazole and lansoprazole were almost equally effective as pantoprazole, yet this drug was most potent on the basis of ED50 values.
[Mh] Termos MeSH primário: Antiulcerosos/uso terapêutico
Benzimidazóis/uso terapêutico
Úlcera Duodenal/tratamento farmacológico
Omeprazol/análogos & derivados
Omeprazol/uso terapêutico
Inibidores da Bomba de Prótons
Sulfóxidos/uso terapêutico
[Mh] Termos MeSH secundário: 2-Piridinilmetilsulfinilbenzimidazóis
Ácido Acético
Animais
Bicarbonatos/metabolismo
Relação Dose-Resposta a Droga
Úlcera Duodenal/induzido quimicamente
Inibidores Enzimáticos/uso terapêutico
Epirizol
Ácido Gástrico/secreção
Lansoprazol
Masculino
Ratos
Ratos Sprague-Dawley
Cicatrização/efeitos dos fármacos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-Pyridinylmethylsulfinylbenzimidazoles); 0 (Anti-Ulcer Agents); 0 (Benzimidazoles); 0 (Bicarbonates); 0 (Enzyme Inhibitors); 0 (Proton Pump Inhibitors); 0 (Sulfoxides); 0K5C5T2QPG (Lansoprazole); 3B46O2FH8I (Epirizole); D8TST4O562 (pantoprazole); KG60484QX9 (Omeprazole); Q40Q9N063P (Acetic Acid)
[Em] Mês de entrada:9906
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990410
[St] Status:MEDLINE


  10 / 74 MEDLINE  
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[PMID]:9892884
[Au] Autor:Takeuchi K; Hirata T; Yamamoto H; Kunikata T; Ishikawa M; Ishihara Y
[Ad] Endereço:Department of Pharmacology and Experimental Therapeutics, Kyoto Pharmaceutical University, Misasagi, Yamashina, Kyoto 607-8414, Japan. takeuchi@mb.kyoto-phu.ac.jp
[Ti] Título:Effects of S-0509, a novel CCKB/gastrin receptor antagonist, on acid secretion and experimental duodenal ulcers in rats.
[So] Source:Aliment Pharmacol Ther;13(1):87-96, 1999 Jan.
[Is] ISSN:0269-2813
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: S-0509, 2-[(tert-butoxycarbonylmethyl) [(m-(carboxy-phenyl)-ureidomethyl-carbonyl]] aminobenzo phenone, was developed as a potent and selective CCKB/gastrin receptor antagonist that does not affect the central nervous system. METHODS: We evaluated the effects of S-0509 on gastric acid secretion and duodenal ulcerogenic and healing responses in rats comparing it with L-365,260, another CCKB/gastrin receptor antagonist. RESULTS: S-0509 (0.1 approximately 10 mg/kg, i.d.) was able to dose-dependently decrease basal acid secretion and inhibit the acid secretory responses induced by both pentagastrin (60 microg/kg/h, i.v.) and peptone (10%, i.g.) but not histamine (4 mg/kg/hr, i.v.) or carbachol (60 microg/kg/h, i.v.). L-365,260 (10 and 30 mg/kg, i.d.) caused only partial a suppression of the acid secretory response to pentagastrin but not to other stimuli, including peptone treatment. On the other hand, a duodenal ulcerogen, mepirizole (200 mg/kg, s.c. ) caused an increase in acid secretion and resulted in penetrating ulcers in the proximal duodenum, and these ulcers gradually healed over 3 weeks. S-0509 significantly inhibited both the acid secretory (> 1.0 mg/kg, i.d.) and ulcerogenic (> 3 mg/kg, p.o.) responses induced by mepirizole when it was given as a pre-treatment. It also promoted significantly the healing of these ulcers (> 3 x 2 mg/kg, p. o.) when it was given twice daily for 14 days. In contrast, L-365, 260 (30 mg/kg) tended to reduce the severity of mepirizole-induced duodenal ulcers, with a slight inhibition of acid secretion, but it caused no influence on the healing response of these ulcers. CONCLUSION: These results confirmed that S-0509 is a selective CCKB/gastrin receptor antagonist with potent antisecretory action in vivo conditions, and further demonstrated that this agent not only prevents the development of duodenal ulcers but also shows healing promoting action on duodenal ulcers, probably through the blockade of CCKB/gastrin receptors.
[Mh] Termos MeSH primário: Benzofenonas/farmacologia
Úlcera Duodenal/fisiopatologia
Compostos de Fenilureia/farmacologia
Receptores da Colecistocinina/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/farmacologia
Benzodiazepinonas/farmacologia
Benzodiazepinonas/uso terapêutico
Benzofenonas/uso terapêutico
Relação Dose-Resposta a Droga
Úlcera Duodenal/tratamento farmacológico
Epirizol/farmacologia
Ácido Gástrico/secreção
Mucosa Gástrica/efeitos dos fármacos
Mucosa Gástrica/secreção
Concentração de Íons de Hidrogênio
Masculino
Pentagastrina/farmacologia
Peptonas/farmacologia
Compostos de Fenilureia/uso terapêutico
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Benzodiazepinones); 0 (Benzophenones); 0 (Peptones); 0 (Phenylurea Compounds); 0 (Receptors, Cholecystokinin); 0 (S 0509); 370JHF4586 (L 365260); 3B46O2FH8I (Epirizole); EF0NX91490 (Pentagastrin)
[Em] Mês de entrada:9903
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990120
[St] Status:MEDLINE



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